Good Entrapment Efficiency Research Articles

Process optimisation, characterisation and evaluation of resveratrol-phospholipid complexes using Box-Behnken statistical design

With the advent of 21st century, researchers worldwide have extensively reviewed herbs and botanicals for their marked clinical efficacy. It has been estimated that most of the newly discovered compounds offer poor bioavailability due to their low aqueous solubility. Phospholipid complexation of the drug often helps to improve its water solubility and enhance the bioavailability. This study includes optimization of resveratrol-phospholipid complexes using a 3-factor, 3-level box-behnken design (15 batches). Three independent variables i.e. phospholipid-resveratrol ratio, refluxing temperature and reflux time were optimized for two dependent variables, i.e. yield and entrapment efficiency (EE). Complexes were prepared by refluxing stoichiometric ratio of Phospholipon 90G and resveratrol in dichloromethane and retrieved by precipitation with n-hexane. Complexation was confirmed by Fourier Transform Infra-Red (FTIR) spectroscopy. The data was suitably used to explore quadratic response surfaces and construct second order polynomial models with Design Expert®. Formulation with highest desirability (D=0.994) was selected as optimum and prepared using 1.5:1 Phospholipon 90G-resveratrol ratio (X1) at 59.4°C temperature (X2) and 4 h time (X3) to give maximum yield and entrapment efficiency. Analysis of variance (ANOVA) was also found to be significant for both the responses. Complexes were optimised for good yield and EE. The partition coefficient was lowered to 2.25 hypothesizing good passive absorption.DOI: http://dx.doi.org/10.3329/icpj.v3i7.19079 International Current Pharmaceutical Journal, June 2014, 3(7): 301-308

Modified Xanthan Gum as Hydrophilic Disintegrating Excipient for Rapidly Disintegrating Tablets of Roxithromycin

Abstract: The main aim of the present work was to fabricate and evaluate gastro retentive high density microspheres with both synthetic and natural polymers for the sustained release of Famotidine to treat gastric ulcers. The microspheres were prepared by the coacervation phase separation technique. Famotidine was checked for its compatibility with polymers used by Fourier Transform Infrared spectroscopy (FTIR). The surface morphology was studied by scanning electron microscopic (SEM) studies. The percentage of yield, surface associated drug content, drug entrapment efficiency and in vitro dissolution studies were performed and the dissolution data was treated with mathematical kinetic models. Accelerated stability studies were also carried out to the optimized formulation (F-6). The FTIR spectrum of pure drug and drug-polymer blend showed the stable character of Famotidine in the micro capsules. The microspheres were found to be spherical. The microspheres had good entrapment efficiency and percentage yield. The release of drug from the microspheres extended up to 12 h. The release kinetics data and characterization studies indicate that drug release from microspheres was diffusion sustained and that the microspheres were stable. The study revealed that Gellan gum and Karaya gum in combinations with Povidone found to be effective combination for microspheres and the gastric retention was aided with Titanium dioxide. Keywords: Famotidine, Microspheres, Gellan gum, Karaya gum, Titanium dioxide.

Albumin nanoparticles coated with polysorbate 80 as a novel drug carrier for the delivery of antiretroviral drug-Efavirenz.

Purpose of the study:The antiretroviral therapy (ART) has dramatically improved human immunodeficiency virus (HIV)/acquired immunodeficiency syndrome (AIDS) treatment, prevention and also has been found to increase the lifespan of HIV/AIDS patients by providing durable control of the HIV replication in patients. Efavirenz is a non-nucleoside reverse transcriptase inhibitor of HIV-1. The purpose of this study is to formulate efavirenz-loaded bovine serum albumin nanoparticles to improve efavirenz delivery into various organs.Materials and Methods:Nanoparticles were prepared by desolvation technique and coated with polysorbate 80. Ethanol, glutaraldehyde, and mannitol were used as desolvating, cross linking agent, and cryoprotectant, respectively. Drug to polymer ratio was chosen at five levels from 1:2, 1:3, 1:4, 1:5, and 1:6 (by weight). The formulated nanoparticles were characterized for Fourier Transform Infrared (FT-IR) spectroscopy, differential scanning calorimetry (DSC) studies, entrapment efficiency, particle size, surface charge, surface morphology, in vitro drug release, release kinetics, stability studies, and biodistribution studies.Results and Major Conclusion:The particle size of the prepared formulations was found below 250nm with narrow size distribution, spherical in shape and showed good entrapment efficiency (45.62-72.49%). The in vitro drug release indicated biphasic release and its data were fitted to release kinetics models and release pattern was Fickian diffusion controlled release profile. The prepared nanoparticles increased efavirenz delivery into various organs by several fold in comparison with the free drug.

Critical analysis of algino-carbopol multiparticulate system for the improvement of flowability, compressibility and tableting properties of a poor flow drug

The objective behind this study is to ameliorate the flowability, compressibility and tableting properties of aceclofenac by developing a prolonged release microparticulate system using an algino-carbopol polymeric blend. Prepared microspheres were subjected to various physico-chemical studies along with in vitro drug release studies to optimize the concentration of the polymeric blend required to sustain the drug release for 12h. Optimize formulation was further subjected to different flowability and compressibility studies to observe the impact of microspheres on improvements of flow properties. All the microsphere formulations exhibited good entrapment efficiency and showed prolonged drug release. SEM study revealed that the microspheres were almost spherical in shape with rough outer surface containing small pores. The findings of micromeritic studies suggested that the flowability and compressibility properties of the pure drug were significantly improved by the microsphere formulation. Heckel analysis also suggested that the microspheres exhibited better plasticity and die filling behavior as compared to pure drug. The tablets containing optimized microspheric formulation showed better handling properties than pure drug and no significant difference in drug release when compared with the marketed product. So the present study concluded that encapsulation of aceclofenac into microparticulate system not only enhanced its flowability, compressibility and tableting properties but also simultaneously helped to improve the patient compliance by sustaining the drug release for a prolonged period of time to manage pain and its symptoms.

FORMULATION AND CHARECTERISATION OF COLON TARGETED pH DEPENDENT MICROSPHERES OF CAPECITABINE FOR COLORECTAL CANCER

The aim of the present work was to prepare the colon-targeting microspheres of capecitabine (CPB) for the treatment of colorectal cancer to reduce dosing frequency and improve patient compliance. PH-sensitive polymer Eudragit L100, S100 separately and in combination (1:2) was used to formulate the microspheres by emulsion solvent diffusion technique using varying drug – polymer ratios (1:2 to 1:6). Microspheres were evaluated for particle size, shape, flow properties, surface morphology by scanning electron microscopy, yield, drug content, and in vitro drug release behavior and found to be significantly affected by polymer concentration. The formulated microspheres were discrete, spherical with relatively smooth surface, and with good flow properties. CPB-loaded microspheres demonstrated good entrapment efficiency (53.28 to 93.76%). The release study was done in simulated gastrointestinal fluids for 2 hrs in SGF (pH 1.2), for 3 hrs in SIF (pH 6.8) and up to 24 hrs in SCF (pH 7.4) and have shown that the drug was protected from being released in the physiological environment of the stomach and small intestine and efficiently released in colon (99.39%). Formulation ELS2 gave the best result among all formulations (1.59% release at end of 2 hrs, 19.24% at the end of 5 hr, and 99.39% at the end of the study). It is concluded from the present study that pH sensitive Eudragit microspheres are promising carriers for oral colon-targeted delivery of CPB for colorectal cancer. Key Words: Capecitabine, Eudragit L-100, Eudragit S-100, microspheres, pH sensitive, colon targeting, colorectal cancer.

Design and development of ethosomal transdermal drug delivery system of valsartan with preclinical assessment in Wistar albino rats

Valsartan (VLT) is a highly selective and orally active antihypertensive drug. However, its oral administration is associated with drawbacks like low bioavailability. The objective of this study was to design and develop a transdermal delivery system for VLT using ethosomal carriers to investigate their enhanced transdermal delivery potential. VLT ethosomes were prepared by cold method. VLT ethosomes were characterized by scanning electron microscopy. The prepared ethanolic liposomes were characterized to be spherical having low polydispersity of nano-size range with good entrapment efficiency. ETC5 ethosomal suspension with 4% of phospholipon 90H and 40% of ethanol was found to have highest entrapment efficiency, i.e. 80.230 ± 0.8748%. The permeation study of ethosomes was evaluated by ex vivo diffusion study through rat abdominal skin using Franz’s diffusion cells and ETC5 ethosomal suspension was found to have highest permeation with flux of 92.819 ± 1.539 µg/cm2/h, when compared to the permeation profiles of drug solutions either in water or in a water–ethanol mixture. Transdermal application of ethosomal VLT on Wistar rats showed better and prolonged antihypertensive activity in comparison to orally administered VLT suspension by virtue of transdermal permeation through Wistar rat skin. Histopathological study of skin applied with ETC5 showed intercellular permeation across skin by dissolving intercellular lipids in epidermis without causing any rigorous changes in the skin cellular structure. In conclusion, ethosomes enabled the transdermal permeation of VLT, which amply proves its superiority over oral administration for antihypertensive treatment.

Antioxidant Activity of Solid Lipid Nanoparticles Loaded with Umbelliferone

The objective of this investigation was to develop solid lipid nanoparticles (SLNs) of umbelliferone by means of a high shear homogenization technique and to evaluate the efficiency of SLN systems in preserving and enhancing antioxidant activity of the flavonoid active component. The aqueous SLN dispersions combine two structural types of lipid compounds and different types of emulsifiers including a mixture of monoalkyl polyoxyethylene sorbitan with a block copolymer and lecithin. The assessment of umbelliferone stability in aqueous SLN dispersions, the size distribution of lipid nanoparticles loaded with umbelliferone (by DLS technique), as well as the structural changes (FT-IR spectroscopy and differential scanning calorimetry) of these lipid nanomatrices have been investigated. Moreover, the influence of umbelliferone concentration onto entrapment efficiency and antioxidant properties were clearly evidenced on four kinds of lipid nanoparticles. The umbelliferone-loaded SLN prepared with polyethylene glycol sorbitan monostearate shown a mean particle size of 173.4 nm ± 3.279, as well as good entrapment efficiency (EE = 60.70%) and antioxidant properties (AA = 75%).

Formulation and Optimization of 5-Fluorouracil Loaded Chitosan Nanoparticles Employing Central Composite Design

5-Fluorouracil (5-FU) is a hydrophilic drug with short plasma half-life. The objective of the current study was to prepare and optimize 5-FU loaded chitosan nanoparticles (CNPs) for controlled release. The nanoparticles were prepared by ionic gelation of chitosan with tripolyphosphate anions. A 23 central composite design (CCD) was employed to study the influence of formulation variables - concentration of Chitosan (X1), the concentration of sodium tripolyphosphate (NaTPP) (X2) and volume of NaTPP (X3) on the cumulative percentage of drug release. The relationship between the dependent and independent variables was further elucidated using multiple linear regression analysis (MLRA) and Pareto chart. The results show that cumulative percent of 5-FU release was highest and lowest at high levels of X1, X2, and low level of X3, and high level of X1, and low levels of X2 and X3, respectively. The optimized nanoparticles were studied morphologically by transmission electron microscopy (TEM) which showed separated and non-aggregated nanoparticles with spherical shapes and smooth surfaces. The mean particle size, entrapment efficiency and loading capacity of the optimal CNPs were found to be 109.6±2.28 nm, 83.84±1.46%, and 37.76±3.41%, respectively. Nanoparticles revealed a fast release during the first hour followed by a more gradual drug release during a 24-h period following a non-Fickian diffusion process. Analysis of variance (ANOVA) was applied on cumulative percent of drug release to study the fitting and significance of model. The estimated model may be further utilized as response surface for cumulative percent of drug release from nanoparticles. The 5-FU loaded CNPs optimized using CCD showed good entrapment efficiency and controlled release as well as can reduce dosing frequency, decrease side effects and improve patient compliance.

Development and characterization of ligand-appended liposomes for multiple drug therapy for pulmonary tuberculosis

Tuberculosis (TB) remains one of the oldest and deadliest diseases in the current scenario. The intracellular organism Mycobacterium tuberculosis, which mainly resides in mononuclear phagocytes, is responsible for tuberculosis in humans. A few therapies are available for the treatment of tuberculosis but they have many hurdles. To overcome these hurdles, a combination of chemotherapeutic agent-loaded vesicular systems have been prepared to overcome tuberculosis. To investigate the role of novel drug delivery systems for the treatment of pulmonary tuberculosis, ligand appended liposomals have been developed. In the present study, drug-loaded, ligand-appended liposomes and their DPI (Dry Powder Inhaler) forms have been prepared and characterized using various in vitro and in vivo parameters. The prepared ligand-appended liposomal formulation showed good entrapment efficiency, prolonged drug release, improved recovery of drugs from the target site, and proved to be more suitable for use as DPI, justifying their potential for improved drug delivery. Thus we tried our best by our project to reduce the national burden of tuberculosis, which is still a global health challenge.

Macrophages targeting of amphotericin B through mannosylated multiwalled carbon nanotubes

The objective of the present investigation was to assess the potential of polysaccharide (mannose) conjugated engineered multiwalled carbon nanotubes (MWCNTs) bearing Amphotericin B (AmB) formulation for site-specific delivery to macrophages. The mannosylated carbon nanotubes (CNTs) were synthesized and AmB was efficiently loaded using dialysis diffusion method. The synthesized mannosylated MWCNTs were characterized by various physicochemical and physiological parameters such as fourier transform infrared (FTIR) spectroscopy, scanning and transmission electron microscopy (SEM & TEM), drug loading and entrapment efficiency, in-vitro release kinetics, in-vivo study and toxicological investigation. AmB loaded mannosylated MWCNTs (AmBitubes) was found to be nanometric in size (500 nm) with tubular structure and good entrapment efficiency (75.46 ± 1.40%). In-vitro AmB from AmBitubes was found to be released in a controlled manner at pH 4, 7.4 and 10, with enhanced cell uptake and higher disposition in macrophage-rich organs, thereby indicating the site-specific drug delivery. The results suggest that AmBitubes could be employed as efficient nano-carrier for antileishmanial therapy.

Preparation of a ligustrazine ethosome patch and its evaluation in vitro and in vivo

BackgroundThe purpose of this study was to develop a transdermal ligustrazine patch containing a stable formulation and with good entrapment efficiency, release rate, and transdermal absorption.MethodsLigustrazine ethosomes were prepared by ethanol injection-sonication, with entrapment efficiency as an indicator. Using acrylic resin as the primary constituent, the ligustrazine ethosome patch was prepared by adding succinic acid as a crosslinking agent and triethyl citrate as a plasticizer. In vitro release and transdermal permeation studies were carried out. Finally, a pharmacokinetic study was carried out in rats to explore relative bioavailability. The formulations of ligustrazine ethosome were 1% (w/v) phospholipid, 0.4% (w/v) cholesterol, and 45% (v/v) ethanol.ResultsLigustrazine ethosomes were obtained with an average particle size of 78.71 ± 1.23 nm and an average entrapment efficiency of 86.42% ± 1.50%. In vitro transdermal testing of the ligustrazine ethosome patches showed that the cumulative 24-hour amount of ligustrazine was up to 183 ± 18 μg/cm2. The pharmacokinetic results revealed that the relative bioavailability was 209.45%.ConclusionCompared with conventional ligustrazine administration, ligustrazine ethosome patches could promote better drug absorption and increase bioavailability. This study demonstrates that the transdermal action of the ligustrazine ethosome patch was comparatively good.

Formulation development and in vitro evaluation of gastroretentive hollow microspheres of famotidine

Background:The main aim of this study was to develop a gastroretentive, multiple-unit floating drug delivery system for a drug which is poorly absorbed from the lower gastrointestinal tract. Such a dosage form may provide an extended retention of drug in the upper gastrointestinal tract resulting in enhanced absorption and improved bioavailability.Materials and Methods:Microspheres were prepared by the emulsion solvent diffusion method. Four different ratios (1:1, 1:2, 1:3, and 1:4) from each polymer, i.e., Eudragit RL 100 (E1–E4) and cellulose acetate (C1–C4) were prepared.Results:Hollow microspheres were characterized by particle size using optical microscopy. The in vitro release data obtained for the formulations E1–E4 and C1–C4 showed good entrapment efficiency, good percentage buoyancy, and prolonged drug release. The in vitro drug release showed the highest regression coefficient values for Higuchi's model, indicating diffusion to be the predominant mechanism of drug release. The surface and cross-sectional morphology of the formulations E1-A and C1-A were determined using scanning electron microscopy.Conclusions:Thus, prepared floating hollow microspheres of famotidine may prove to be potential candidates for the multiple-unit drug delivery device adaptable for any intragastric condition.

Transcutol containing vesicles for topical delivery of minoxidil

The aim of this work was to evaluate the ability of Transcutol (Trc) to produce elastic vesicles with soy lecithin (SL) and study the influence of the obtained vesicles on in vitro (trans)dermal delivery of minoxidil. To this purpose, so-called penetration enhancer-containing vesicles (PEVs) were prepared using Trc aqueous solutions (5–10–20–30% v/v) as hydrophilic phase. SL liposomes, without Trc, were used as control. Prepared formulations were characterized in terms of size distribution, morphology, zeta potential, deformability, and rheological behavior. The influence of the obtained PEVs on (trans)dermal delivery of minoxidil was studied by in vitro diffusion experiments through pig skin. Results showed that all prepared PEVs were able to give good entrapment efficiency (E%≈67) similar to that of conventional liposomes. Trc-containing PEVs showed to be more deformable than liposomes only when minoxidil was loaded in 5 and 10% Trc-containing vesicles. Rheological studies showed that PEVs have higher fluidity than conventional liposomes. All PEVs showed a higher stability than liposomes as shown by studying zeta potential and size distribution during three months. Results of in vitro diffusion experiments showed that Trc-containing PEVs are able to deliver minoxidil to deep skin layers without any transdermal permeation.

Electrospray technique for solid lipid-based particle production

Background: Different preparation methods for the production of lipid micro- and nanoparticles as controlled release formulations have been widely developed. Novel techniques are attracting increasing attention for their preparation. Method: The objective of the present investigation was to produce solid lipid-based micro-nanospheres using the electrohydrodynamic atomization (electrospraying) and to evaluate whether it is a suitable method to prepare drug-loaded particles. Results: Narrowly dispersed spherical particles lower than 1 μm, easily internalized in cells, were obtained using stearic acid and ethylcellulose in a 4.5:0.5 (w/w) ratio. Tamoxifen, as model drug, was encapsulated with good entrapment efficiency. The in vitro release, after an initial burst effect, showed a prolonged drug release. Conclusion: The electrospraying method might be proposed to prepare in a single-step monodisperse lipid-based micro- and nanoparticles in powder form for drug delivery.

Preparation, Characterization and Evaluation of Targeting Potential of Amphotericin B-Loaded Engineered PLGA Nanoparticles

The objective of present work was to develop a mannose-anchored, engineered nanoparticulate system for efficient delivery of amphotericin B to macrophages. Furthermore, the effect of spacer on macrophage targeting was also evaluated. PLGA was conjugated to mannose via direct coupling (M-PLGA) and via PEG spacer (M-PEG-PLGA), and engineered PLGA nanoparticles (M-PNPs and M-PEG-PNPs) were prepared from respective conjugates. These prepared engineered PNPs were characterized for size, polydispersity index (PDI), surface charge, and drug entrapment efficiency (% DEE). Transmission electron microscopy (TEM) and atomic force microscopy (AFM) were employed to study the shape and surface morphology of engineered PNPs. Macrophage targeting was evaluated via cellular uptake, ex vivo antileishmanial activity and in vivo biodisposition pattern of engineered PNPs in macrophage-rich organs. The developed engineered PNPs were found to be of nanometric size (<200 nm) and to have low PDI (<0.162) and good entrapment efficiency (%DEE >53.0%). AFM and TEM revealed that both M-PNPs and M-PEG-PNPs had smooth surface and spherical topography. Engineered PNPs with spacer showed enhanced uptake, potential antileishmanial activity and higher disposition in macrophage-rich organs, suggesting improved macrophage targeting. The results suggest that engineering of nanoparticles could lead to development of efficient carrier for macrophage targeting.

Calcium Pectinate Gel Bead Intended for Oral Protein Delivery: Preparation Improvement and Formulation Development

Calcium pectinate gel (CPG) micrometer-sized beads (microbeads) containing insulin, as a model amphoteric protein, were prepared by ionotropic gelation technique together with an air compressor. The influences of phosphate buffer, pH as well as calcium and pectin concentrations of cross-linking solution on the characteristics and release profiles of microbeads were investigated. With the aid of compressed air flow, the mean diameters of beads were successfully decreased to micron-sized. The results showed that all the factors investigated greatly affected the entrapment efficiencies and release profiles of the microbeads. Suitable formulation concentrations should be considered and great care should be taken to maintain the pH of working solutions at or close to isoelectric point of protein loaded during the whole preparation process. Hence, CPG microbeads of perfect spherical shape, uniform sizes, enhanced mechanical strength, good entrapment efficiencies and delayed release profiles were prepared for a load of amphoteric protein and peptide drugs, without any use of organic solvents or harsh ingredients. Therefore, CPG microbeads could be a promising carrier for oral controlled-release systems of amphoteric protein and peptide drugs.

Gel core liposomes: An advanced carrier for improved vaccine delivery

Many sub-unit vaccines are successful in preventing the occurrence of disease, but their use is largely restrained due to low immunogenicity. Novel carrier-based vaccine could serve as a vaccine adjuvant to overcome low immunogenicity of sub-unit vaccines. The use of liposomes as a delivery system for antigen is well recognized but they are unstable and release of antigen from them cannot be controlled over a prolonged period of time. To overcome the limitation of liposomes, this study has developed gel core liposomes in which a core of polymer was incorporated inside the liposomal vesicles, which serve the function of skeleton and provide mechanical strength to vesicles. In the present investigation BSA-loaded gel core liposomes were prepared by reverse phase evaporation method and characterized for vesicles size, shape, entrapment efficiency, in vitro release and stability studies. The in vivo studies to evaluate antigen presenting potential of the gel-core liposomes was performed in Balb/c mice by measuring the immune response elicited by intramuscular administration of BSA-loaded gel core liposomes and compared with intramuscularly administered BSA-loaded conventional liposomes, alum adsorbed BSA and plain antigen. Results indicate that intramuscular immunization with gel core liposomes induces efficient systemic antibody responses against BSA as compared to other formulations. The gel core liposomal formulation provides good entrapment efficiency, enhanced in vitro stability, prolonged antigen release and effective immunoadjuvant property, justifying its potential for improved vaccine delivery.

Development, characterization, and toxicity evaluation of amphotericin B–loaded gelatin nanoparticles

Our aim in the present investigation was to develop a nanoparticulate carrier of amphotericin B (AmB) for controlled delivery as well as reduced toxicity. Nanoparticles of different gelatins (GNPs) (type A or B) were prepared by two-step desolvation method and optimized for temperature, pH, amount of cross-linker, and theoretical drug loading. AmB-loaded GNPs were characterized for size, polydispersity index (PI), shape, morphology, surface charge, drug release, and hemolysis. The developed GNPs (GNP A300) were found to be of nanometric size (213 ± 10 nm), having low PI (0.092 ± 0.015) and good entrapment efficiency (49.0 ± 2.9%). All GNPs showed biphasic release characterized by an initial burst followed by controlled release. The in vivo hematological toxicity results suggest nonsignificant reduction ( P > .05) in hemoglobin concentration and hematocrit. Nephrotoxicity results showed that there was a nonsignificant ( P > .05) increase in blood urea nitrogen and serum creatinine levels. The results confirm that developed GNPs could optimize AmB delivery in terms of cost and safety, and type A gelatin with bloom number 300 was found suitable for such preparation.

Etoposide-Loaded PLGA and PCL Nanoparticles I: Preparation and Effect of Formulation Variables

Etoposide-loaded nanoparticles were prepared using nanoprecipitation and emulsion solvent evaporation techniques using polylactide-co-glycolic acid and poly(ε -caprolactone) in presence of Pluronic F68, respectively. Effect of formulation variables like stabilizer concentration, amount of polymer, and drug was studied. These parameters were found to affect particle size, zeta potential, drug content, and entrapment efficiency of nanoparticles. The methods produced nanoparticles with good entrapment efficiency of around 80%. Recovery of nanoparticles was as high as 95% and drug content was around 1.5%. Increase in lactide content decreased the release of etoposide in vitro and poly(ε -caprolactone) nanoparticles retarded etoposide release for 48 hr. The results show the suitability of polylactide-co-glycolic acid and poly(ε -caprolactone) nanoparticles as potential carriers for controlled delivery of etoposide.

Development of potent oral nanoparticulate formulation of coenzyme Q10 for treatment of hypertension: Can the simple nutritional supplements be used as first line therapeutic agents for prophylaxis/therapy?

Coenzyme Q10 (CoQ10) is an antioxidant with well-established pharmacological activities against several chronic diseases; however, it is marketed only as a nutritional supplement without any claims of its therapeutic activity and one of the reasons for this could be the poor oral bioavailability rendering difficulties in administering this molecule to achieve therapeutic concentrations. Therefore, the present investigation was aimed at improving the oral bioavailability of CoQ10 by delivering it as nanoparticulate formulation. Biodegradable nanoparticulate formulations based on poly(lactide-co-gylcolide) (PLGA) were prepared by emulsion technique using quaternary ammonium salt didodecyldimethylammonium bromide (DMAB) as a stabilizer. The effect of initial CoQ10 loading on entrapment efficiency and the particle size was studied using 5–75% initial load resulting in good entrapment efficiency (61–83%) without any appreciable increase in the particle size for 5–30% loading (107–110 nm). However, 50% and 75% led to increase in particle size with no appreciable changes in entrapment efficiency. The intestinal uptake of CoQ10 as a suspension in carboxymethylcellulose (CMC), a commercial formulation and the developed nanoparticulate formulation was studied in male Sprague–Dawley (SD) rats and found to be 45%, 75% and 79%, respectively, suggesting that solubility and permeability related problems of CoQ10 were overcome by nanoparticulate formulation. Furthermore, the developed nanoparticulate formulation was evaluated for its therapeutic potential in renal hypertensive animals (Goldblatt 2K1C model), demonstrating improved efficacy at a 60% lowered dose as compared to CoQ10 suspension and superior efficacy than the commercial formulation at an equal dose. Together, these results indicate the potential of nanotechnology in improving the therapeutic value of molecules like CoQ10, facilitating its usage as first line therapeutic agent thus revolutionizing its role in current medical therapy.